Piqray (Alpelisib) - Oral

What Is Piqray?

Piqray (alpelisib) is an oral medication used to treat certain types of breast cancer that are metastatic (spread to other areas of the body).

It is in a class of medications called kinase inhibitors, which work by inhibiting certain pathways in the cancer cells that signal them to grow.

Alpelisib is available by prescription in tablet form.

Drug Facts

Generic Name: Alpelisib

Brand Name(s): Piqray

Drug Availability: Tablets

Administration Route: Oral

Therapeutic Classification: Kinase inhibitor

Available Generically: No

Controlled Substance: N/A

Active Ingredient: Alpelisib

Dosage Form(s): Tablets

What Is Piqray Used For?

Piqray is used in combination with another medication called fulvestrant in adults to treat:

A PIK3CA mutation can be found with specialized genetic testing done on the cancer cells. About 40% of HR-positive, HER2-negative metastatic breast cancers will have a mutation in the PIK3CA gene.

When the PIK3CA gene is functioning normally, the protein signal for cells tells the cells to grow and divide normally. However, when the gene is mutated, the protein signal is too fast and irregular, causing cells to grow out of control.

Piqray works by blocking some of those abnormal signals to normalize cell growth.

How to Take Piqray

Piqray should be taken once a day, with food, and around the same time. 

Swallow the tablets whole; do not crush, break, or chew them.


Keep Piqray at room temperature (between 68 F and 77 F) and out of the reach of children and pets. Do not store it in the bathroom. The medication comes in a blister pack and should remain in the pack until ready to be taken.

How Long Does Piqray Take to Work?

Piqray is typically used as a long-term treatment to prolong survival without disease progression and shrink cancer tumors. Your cancer care team will determine how long you'll need to be on this therapy.

What Are the Side Effects of Piqray?

This is not a complete list of side effects, and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your healthcare provider or pharmacist. You may report side effects to the Food and Drug Administration (FDA) at www.fda.gov/medwatch or 800-FDA-1088.

Common Side Effects

The most common side effects that are experienced with taking Piqray include:

Piqray may also cause abnormal lab test results, such as:

Severe Side Effects

Call your healthcare provider immediately if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

  • Allergic reaction: Rash, fever, flushing, fast heartbeat
  • Severe skin reaction: Blistering, peeling, redness of the skin
  • High blood sugar level (hyperglycemia): Severe thirst, frequent urination, dry mouth, weight loss
  • Pneumonitis (lung inflammation): Shortness of breath, cough, chest pain
  • Diarrhea

Because of the risk of hyperglycemia, your healthcare provider may recommend frequent monitoring of your blood glucose levels and hemoglobin A1c.

Report Side Effects

Piqray may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your healthcare provider may send a report to the FDA's MedWatch Adverse Event Reporting Program or by phone (800-332-1088).

Dosage: How Much Piqray Should I Take?

Drug Content Provided and Reviewed by IBM Micromedex®

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For breast cancer:
      • Adults—300 milligrams (mg) (two 150 mg tablets) once a day. Your doctor may adjust your dose as needed and tolerated.
      • Children—Use and dose must be determined by your doctor.
    • For PIK3CA-related overgrowth spectrum (PROS):
      • Adults—250 milligrams (mg) once a day. Your doctor may adjust your dose as needed and tolerated.
      • Children 6 years of age and older—At first, 50 mg once a day. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 125 mg once a day.
      • Children 2 to younger than 6 years of age—50 mg once a day. Your doctor may adjust your dose as needed and tolerated.
      • Children younger than 2 years of age—Use and dose must be determined by your doctor.


Certain factors may affect whether you take Piqray or how you take it:

  • Side effects: The dose may be changed if any side effects are severe.
  • Breastfeeding: Do not breastfeed during treatment with Piqray and for one week after the last dose.
  • Pregnancy: Piqray can cause harm to the fetus when taken during pregnancy. Use effective contraception during your treatment and for one week after the last dose.

Missed Dose 

If you miss a dose, take the missed dose within nine hours of the time it's normally taken. If it is after nine hours, skip the missed dose. Never double up to make up for a missed dose.

Overdose: What Happens If I Take Too Much Piqray?

In the few reported cases of an overdose of Piqray, the symptoms experienced were similar to the side effects of the medication. Immediately notify your healthcare provider if you take more Piqray than prescribed.

What Happens If I Overdose on Piqray?

If you think you or someone else may have overdosed on Piqray, call a healthcare provider or the Poison Control Center (800-222-1222).

If someone collapses or isn't breathing after taking Piqray, call 911 immediately.


Drug Content Provided and Reviewed by IBM Micromedex®

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood tests may be needed to check for unwanted effects.

It is unlikely that a postmenopausal woman may become pregnant. But, using this medicine while you are pregnant can harm your unborn baby. If you are a woman who can bear children, your doctor may give you a pregnancy test before you start using this medicine to make sure you are not pregnant. Use an effective form of birth control to keep from getting pregnant during treatment and for 1 week after your last dose. Male patients who have female partners should use effective birth control during treatment and for 1 week after the last dose. If you think you have become pregnant while using the medicine, tell your doctor right away.

This medicine may cause serious allergic reactions, including anaphylaxis, angioedema, and anaphylactic shock, which can be life-threatening and require immediate medical attention. Tell your doctor right away if you have a rash, itching, hoarseness, large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth after using this medicine.

This medicine may cause serious skin reactions, including Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, and drug reaction with eosinophilia and systemic symptoms (DRESS). Check with your doctor right away if you have black, tarry stools, blistering, peeling, or loosening of the skin, chest pain, chills, cough, diarrhea, itching, joint or muscle pain, painful or difficult urination, red irritated eyes, red skin lesions, often with a purple center, sore throat, sores, ulcers, or white spots in the mouth or on the lips, swollen glands, trouble breathing, unusual bleeding or bruising, or unusual tiredness or weakness with this medicine.

This medicine may affect your blood sugar levels. Check with your doctor right away if you have increased thirst or increased urination. If you notice a change in the results of your urine or blood sugar tests, or if you have any questions, check with your doctor.

This medicine may cause swelling of the lungs (pneumonitis) or interstitial lung disease. These are life-threatening conditions and require immediate medical attention. The symptoms may be similar to the symptoms from lung cancer. Check with your doctor right away if you have new or worsening cough, fever, or trouble breathing.

This medicine may cause diarrhea (colitis), and in some cases it can be severe. Your doctor may give you medicine to treat diarrhea. Drink plenty of fluids to prevent dehydration and kidney problems. If you have any questions about this or if mild diarrhea continues, or gets worse, check with your doctor. Call your doctor right away if you have stomach pain, or mucus or blood in your stool.

If you plan to have children, talk with your doctor before using this medicine. Some men and women using this medicine have become infertile (unable to have children).

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

What Are Reasons I Shouldn’t Take Piqray? 

You should not take this medication if:

  • You are allergic to the medication or any of its ingredients
  • Are pregnant or breastfeeding (wait at least one week after your last dose to start breastfeeding)

What Other Medications Interact With Piqray?

Some medications should not be taken along with Piqray. Be sure your oncologist has an updated list of all medications that you are taking, including prescription and over-the-counter (OTC) drugs, vitamins, and herbal supplements.

Piqray should not be taken along with the following medications:

What Medications Are Similar?

Piqray is the only medication that targets the PIK3CA pathway to treat metastatic breast cancer.

Frequently Asked Questions

  • What is Piqray used for?

    Piqray is used to treat metastatic HR+, HER2- breast cancer that has been treated with hormone therapy previously. It is used along with another medication called fulvestrant. 

  • How does Piqray work?

    Cancer cells with a PIK3CA mutation can send abnormal signals, which tell the cancer cells to grow out of control. Piqray works by blocking some of those signals to slow cell growth.

  • What are the side effects of Piqray?

    Some of the side effects of Piqray include:

    • Nausea and/or vomiting
    • Diarrhea
    • Feeling tired or weak
    • Hair loss
    • Rash
    • Decreased appetite

How Can I Stay Healthy While Taking Piqray?

As with all medications, Piqray has the potential to cause side effects, some of which can sound concerning. Talk to your cancer care team if you’re prescribed Piqray and have concerns. Often, they can help you work through how to manage any side effects and can answer any questions you have about the medication.

Coping with a breast cancer diagnosis can be overwhelming. Never be afraid to let your healthcare team know how you're feeling. Consider confiding in family, friends, or a support group to help you navigate the emotional and physical aspects of your cancer journey. Additionally, eating a healthy diet and exercising can help make you feel better and keep you healthy even after your treatment.

Medical Disclaimer

Verywell Health's drug information is meant for educational purposes only and is not intended to replace medical advice, diagnosis, or treatment from a healthcare provider. Consult your healthcare provider before taking any new medication(s). IBM Watson Micromedex provides some of the drug content, as indicated on the page.

3 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
  1. DailyMed. Label: Piqray- alpelisib tablet. Piqray- alpelisib kit.

  2. Fusco N, Malapelle U, Fassan M, et al. PIK3CA mutations as a molecular target for hormone receptor-positive, her2-negative metastatic breast cancerFront Oncol. 2021;11:644737. doi:10.3389/fonc.2021.644737

  3. Wilhoit T, Patrick JM, May MB. Alpelisib: a novel therapy for patients with PIK3CA-mutated metastatic breast cancer. J Adv Pract Oncol. 2020;11(7):768-775. doi:10.6004/jadpro.2020.11.7.9

By Julie Scott, MSN, ANP-BC, AOCNP
Julie is an Adult Nurse Practitioner with oncology certification and a healthcare freelance writer with an interest in educating patients and the healthcare community.